title: Synthesis and evaluation of some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives as cytotoxic agents: structure/activity studies.
abstract: Using pregnenolone and 7-deoxycholic acid as starting materials, some 17-acetamidoandrostane and N,N-dimethyl-7-deoxycholic amide derivatives were synthesized. The cytotoxicity of the synthesized compounds was tested in vitro against two tumor cell lines: SGC 7901 (human gastric carcinoma) and Bel 7404 (human liver carcinoma). The result showed that the blockage of the interaction of the amide group with outside groups might cause a decrease of the cytotoxicity, and an O-benzyloximino group at the 3-position of N,N-dimethyl-7-deoxycholic amide could enhance the cytotoxic activity of the compound. The information obtained from the studies provides the structure-activity relationship for these compounds and may be useful for the design of novel chemotherapeutic drugs.
authors.affiliation: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, China.
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Huang
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cui
authors.forename: Linyi
authors.initials: L
authors.lastname: Jia
authors.forename: Chunfang
authors.initials: C
authors.lastname: Gan
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
authors.forename: Chun
authors.initials: C
authors.lastname: Zeng
authors.forename: Aimin
authors.initials: A
authors.lastname: Zhou
mesh_terms: D000731:Androstanes / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003840:Deoxycholic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D055808:Drug Discovery; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: C586207:17-acetamidoandrostane; D000731:Androstanes; D000970:Antineoplastic Agents; C586206:N,N-dimethyl-7-deoxycholic amide; D003840:Deoxycholic Acid